TABLE 5

Concentration of KAE609 and its metabolites in human semen after an oral dose of 300 mg [14C] KAE609

The semen samples were extracted and analyzed by LC-MS/MS for metabolic profiling. The HPLC separation of KAE609 and metabolites was performed using a Zorbax SB-C18 column, as described in the Materials and Methods.

Metabolite/SubjectConcentration of KAE609 and Metabolites in Human Semena
510151025103510451055106MeanSD
ngEq⋅h/ml
M16634287807433231518485216
M1828320322820816226322444
M20.8NDND548198ND189312205
M21.8823123279143ND173308294
M234699164040234050653233229001599
M32ND7526997219304193102
M48ND61331115231287205114
KAE60911493821138475167369613423
Total75882772762357171663443549662470
  • ND, not detectable.

  • a Semen samples were collected from subjects 5103 and 5106 at 6 hours postdose, subjects 5101 and 5105 at 12 hours postdose, and subjects 5102 and 5104 at 24 hours postdose.